RS53669B1 - Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes - Google Patents

Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes

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Publication number
RS53669B1
RS53669B1 RS20140639A RSP20140639A RS53669B1 RS 53669 B1 RS53669 B1 RS 53669B1 RS 20140639 A RS20140639 A RS 20140639A RS P20140639 A RSP20140639 A RS P20140639A RS 53669 B1 RS53669 B1 RS 53669B1
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Serbia
Prior art keywords
alkyl
halogen
group
individually selected
unsubstituted
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RS20140639A
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Serbian (sr)
Inventor
Cosimo Dolente
Patrick Schnider
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F.Hoffmann-La Roche Ag
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Publication of RS53669B1 publication Critical patent/RS53669B1/en

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    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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Abstract

Jedinjenje formule Iu kojojR1 je odabran iz grupe koju čine:i) H,ii) - C1-6-alkil, nesupstituisan ili supstituisan sa 1 do 5 supstituenata pojedinačno odabranih iz grupe koju čine: OH, halogen, cijano i C1-6-alkoksi,iii) -S(O)2- C1-6-alkil, gde je C1-6-alkil nesupstituisan ili supstituisan sa 1 do 5 supstituenata pojedinačno odabranih iz grupe koju čine: OH, halogen, cijano i -alkoksi,iv) -C(O)- C1-6-alkil, gde je C1-6-alkil nesupstituisan ili supstituisan sa 1 do 5 supstituenata pojedinačno odabranih iz grupe koju čine: OH, halogen, cijano i C1-6-alkoksi,v) -C(O)O-C1-6-alkil, gde je C1-6-alkil nesupstituisan ili supstituisan sa 1 do 5 supstituenata pojedinačno odabranih iz grupe koju čine: OH, halogen, cijano i C1-6-alkoksi;vi) cikloalkil, nesupstituisan ili supstituisan sa 1 do 5 supstituenata pojedinačno odabranih iz grupe koju čine: OH, halogen, cijano i C1-6-alkoksi,vii) -S(O)2-(CH2)q-NRiRii, gdeq je 0 ili 1,Ri i Rii su, svaki pojedinačno, odabrani iz grupe koju čine H i C1-6-alkil, ili Ri i Rii obrazuju, zajedno sa azotom za koji su vezani, 3- do 7-člani heterociklil koji sadrži jedan ili dva heteroatoma pojedinačno odabrana od N, O i S, a heterociklil je nesupstituisan ili je supstituisan sa 1 do 5 supstituenata pojedinačno odabranih iz grupe koju čine okso, halogen, C1-6 -alkil i C1-6 -alkoksi,viii) -(CH2)r-NRiiiRiv, gder je 1, 2 ili 3,Riii i Riv su, svaki pojedinačno, odabrani iz grupe koju čine H i C1-6 -alkil, ili Riii i Riv obrazuju, zajedno sa azotom za koji su vezani, 3- do 7-člani heterociklil koji sadrži jedan ili dva heteroatoma pojedinačno odabrana od N, O i S, a heterociklil je nesupstituisan ili je supstituisan sa 1 do 5 supstituenata pojedinačno odabranih iz grupe koju čine okso, halogen, C1-6-alkil i C1-6-alkoksi, iix) -C(O)(CH2)s-NRvRvi, gdes je 1, 2 ili 3,Rv i Rvi su, svaki pojedinačno, odabrani iz grupe koju čine H i C1-6-alkil, ili Rv i Rvi obrazuju, zajedno sa azotom za koji su vezani, 3- do 7-člani heterociklil koji sadrži jedan ili dva heteroatoma pojedinačno odabrana od N, O i S, a heterociklil je nesupstituisan ili je supstituisan sa 1 do 5 supstituenata pojedinačno odabranih iz grupe koju čine okso, halogen, C1-6-alkil i C1-6-alkoksi;R2 je halogen;R3 je 5-člani heteroaril, nesupstituisan ili supstituisan sa (R*)n, pri čemu je svaki R* pojedinačno odabran iz grupe koju čine: halogen, C1-6-alkil, halogen- C1-6-alkil i hidroksi- C1-6-alkil, a gde jen=1, 2 ili 3;i dva susedna R* mogu formirati prsten od 4, 5, 6 ili 7 C;ili njegova famaceutski prihvatljiva so.Prijava sadrži još 14 patentnih zahteva.A compound of formula I wherein R 1 is selected from the group consisting of: i) H, ii) - C 1-6 alkyl, unsubstituted or substituted with 1 to 5 substituents individually selected from the group consisting of: OH, halogen, cyano and C 1-6 alkoxy , iii) -S (O) 2- C 1-6 alkyl, wherein C 1-6 alkyl is unsubstituted or substituted with 1 to 5 substituents individually selected from the group consisting of: OH, halogen, cyano and -alkoxy, iv) - C (O) -C1-6-alkyl, wherein C1-6-alkyl is unsubstituted or substituted with 1 to 5 substituents individually selected from the group consisting of: OH, halogen, cyano and C1-6-alkoxy, v) -C O) O-C1-6-alkyl, wherein C1-6-alkyl is unsubstituted or substituted with 1 to 5 substituents individually selected from the group consisting of: OH, halogen, cyano and C1-6-alkoxy, vi) cycloalkyl, unsubstituted or substituted with 1 to 5 substituents individually selected from the group consisting of: OH, halogen, cyano and C 1-6 alkoxy, vii) -S (O) 2- (CH 2) q -NR 1 R 14, wherein q is 0 or 1, R 1 and R 11 are each selected from the group consisting of H and C1-6-alkyl 1, or R 1 and R 1 form, together with the nitrogen to which they are attached, a 3- to 7-membered heterocyclyl containing one or two heteroatoms individually selected from N, O and S, and the heterocyclyl is unsubstituted or substituted by 1 to 5 substituents individually selected from the group consisting of oxo, halogen, C1-6-alkyl and C1-6 -alkoxy, viii) - (CH2) r-NRiiiRiv, where 1, 2 or 3, R1 and Riv are each selected from groups consisting of H and C1-6-alkyl, or R1 and R1 form, together with the nitrogen to which they are attached, a 3- to 7-membered heterocyclyl containing one or two heteroatoms individually selected from N, O and S, and the heterocyclyl is unsubstituted or substituted by 1 to 5 substituents individually selected from the group consisting of oxo, halogen, C1-6-alkyl and C1-6-alkoxy, iix) -C (O) (CH2) s-NRvRvi, where 1, 2 or 3, Rv and Rvi are each independently selected from the group consisting of H and C1-6-alkyl, or Rv and Rvi form, together with the nitrogen to which they are attached, a 3- to 7-membered heterocyclyl containing one or two h eteroatom individually selected from N, O and S, and heterocyclyl is unsubstituted or substituted with 1 to 5 substituents individually selected from the group consisting of oxo, halogen, C1-6-alkyl and C1-6-alkoxy, R2 is halogen, R3 is halogen 5-membered heteroaryl, unsubstituted or substituted with (R *) n, each R * being individually selected from the group consisting of: halogen, C1-6-alkyl, halogen-C1-6-alkyl and hydroxy-C1-6- alkyl, and wherein yen = 1, 2 or 3, and two adjacent R * may form a ring of 4, 5, 6 or 7 C, or a pharmaceutically acceptable salt thereof.

RS20140639A 2010-05-10 2011-05-09 Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes RS53669B1 (en)

Applications Claiming Priority (2)

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EP10162451 2010-05-10
PCT/EP2011/057368 WO2011141396A1 (en) 2010-05-10 2011-05-09 Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes

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RS53669B1 true RS53669B1 (en) 2015-04-30

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EP (1) EP2569319B1 (en)
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CA2739900C (en) 2008-11-18 2016-11-08 F. Hoffmann-La Roche Ag Alkylcyclohexylethers of dihydrotetraazabenzoazulenes
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US8513238B2 (en) 2013-08-20
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BR112012028763A2 (en) 2016-07-19
UA110616C2 (en) 2016-01-25
EA201291187A1 (en) 2013-04-30
DK2569319T3 (en) 2014-10-20
HK1176934A1 (en) 2013-08-09
EP2569319B1 (en) 2014-09-24
AU2011252116B2 (en) 2014-03-13
MA34252B1 (en) 2013-05-02
SG185484A1 (en) 2012-12-28
JP5868959B2 (en) 2016-02-24
PT2569319E (en) 2014-11-24
CN102884065A (en) 2013-01-16
AU2011252116A1 (en) 2012-11-22
TW201200520A (en) 2012-01-01
MY160517A (en) 2017-03-15
AR081374A1 (en) 2012-08-29
US20110275801A1 (en) 2011-11-10
PE20130401A1 (en) 2013-04-10
CL2012003132A1 (en) 2013-06-28
ECSP12012291A (en) 2012-12-28
EP2569319A1 (en) 2013-03-20
SI2569319T1 (en) 2014-12-31
NZ603223A (en) 2014-09-26
CA2797920A1 (en) 2011-11-17
PL2569319T3 (en) 2015-03-31
TWI419892B (en) 2013-12-21
CR20120542A (en) 2013-01-11
IL222815A (en) 2014-08-31
CY1115820T1 (en) 2017-01-25
EA021441B1 (en) 2015-06-30
CO6620058A2 (en) 2013-02-15
WO2011141396A1 (en) 2011-11-17
CN102884065B (en) 2015-11-25
MX2012012857A (en) 2012-11-29
ZA201208317B (en) 2014-04-30
KR20130109958A (en) 2013-10-08
JP2013526500A (en) 2013-06-24

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